Mucins are extensively O-glycosylated proteins that are predominantly expressed by epithelial cells. The secreted and membrane-bound mucins form a physical barrier that protects the apical borders of epithelial cells from damage induced by toxins, microorganisms and other forms of stress that occur at the interface with the external environment. The transmembrane mucin 16 can also signal to the interior of the cell through its cytoplasmic domain.
Available evidence indicates that human carcinomas have exploited MUC16 function in promoting tumorigencity. In this context, with transformation and loss of polarity, MUC16 is expressed at high levels on the entire cell surface in carcinomas of the ovaries. Other work has shown that overexpression of MUC16 confers anchorage-independent growth and tumorigenicity.
Thus a need exists for compounds that selectively target and kill MUC16 expressing tumors.